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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Modeling of Dopamine D2 Receptor - Overview of 35-Year Evolution

Author(s): Vladimir Sukalovic, Vukic Soskic and Sladjana Kostic-Rajacic

Volume 22 , Issue 25 , 2015

Page: [2972 - 2990] Pages: 19

DOI: 10.2174/0929867322666150716114316

Price: $65


Research on dopamine (DA) and its receptors, and in particular the D2 receptor subclass, has been an intriguing and fast developing scientific field in the past 35 years. Methods of medicinal chemistry, molecular and structural biology as well as computational chemistry were used in the studies of DA receptors (DRs). Early attempts to describe DRs were based on a small amount of experimental data available and produced crude models at best. Once crystal structures of bacteriorhodopsin, rhodopsine, various G-protein coupled receptors, and finally D3 DR receptor became available, better and more detailed D2 DR receptor models emerged. These models gave us an insight into the mechanism of ligand-receptor interactions, and paved the way for the synthesis of new dopaminergic compounds, both agonists and antagonists and possible drugs for the treatment of different imbalances of the dopaminergic system. This review covers the key discoveries on the path to the creation of the D2 DR receptor model.

Keywords: 3D structure, computational chemistry, dopamine, GPCR, homology modeling, receptor.

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